Details of the Drug

General Information of Drug (ID: DMF0NQR)

• Drug Name: Eplerenone
• Synonyms: Epoxymexrenone; Inspra; Selara; CGP-30083; Inspra (TN); SC-66110; Eplerenone (JAN/USAN/INN); Inspra, Epoxymexrenone, CGP30083, SC-66110,Eplerenone; 7alpha-methoxycarbonyl-3-oxo-9,11alpha-epoxy-17alpha-pregn-4-ene-21,17-carbolactone

Indication

Disease Entry	ICD 11	Status	REF
Heart failure	BD10-BD13	Approved	[1]
Coronavirus Disease 2019 (COVID-19)	1D6Y	Investigative	[2]

• Therapeutic Class: Antihypertensive Agents
• Affected Organisms: Humans and other mammals
• ATC Code:
  C03DA04: Eplerenone
  C03DA: Aldosterone antagonists
  C03D: ALDOSTERONE ANTAGONISTS AND OTHER POTASSIUM-SPARING AGENTS
  C03: DIURETICS
  C: CARDIOVASCULAR SYSTEM
• Drug Type: Small molecular drug
• #Ro5 Violations (Lipinski): 0:
  Molecular Weight (mw); 414.5
  Logarithm of the Partition Coefficient (xlogp); 1.4
  Rotatable Bond Count (rotbonds); 2
  Hydrogen Bond Donor Count (hbonddonor); 0
  Hydrogen Bond Acceptor Count (hbondacc); 6
• ADMET Property:
  BDDCS Class: Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 2: low solubility and high permeability [3]
  Bioavailability: 69% of drug becomes completely available to its intended biological destination(s) [4]
  Elimination: 3% of drug is excreted from urine in the unchanged form [3]
  MRTD: The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 1.723 micromolar/kg/day [5]
• Chemical Identifiers:
  Formula: C24H30O6
  IUPAC Name: methyl (1R,2S,9R,10R,11S,14R,15S,17R)-2,15-dimethyl-5,5'-dioxospiro[18-oxapentacyclo[8.8.0.01,17.02,7.011,15]octadec-6-ene-14,2'-oxolane]-9-carboxylate
  Canonical SMILES: C[C@]12CCC(=O)C=C1C[C@H]([C@@H]3[C@]24[C@H](O4)C[C@]5([C@H]3CC[C@@]56CCC(=O)O6)C)C(=O)OC
  InChI: InChI=1S/C24H30O6/c1-21-7-4-14(25)10-13(21)11-15(20(27)28-3)19-16-5-8-23(9-6-18(26)30-23)22(16,2)12-17-24(19,21)29-17/h10,15-17,19H,4-9,11-12H2,1-3H3/t15-,16+,17-,19+,21+,22+,23-,24-/m1/s1
  InChIKey: JUKPWJGBANNWMW-VWBFHTRKSA-N
• Cross-matching ID:
  PubChem CID: 443872
  ChEBI ID: CHEBI:31547
  CAS Number: 107724-20-9
  UNII: 6995V82D0B
  DrugBank ID: DB00700
  TTD ID: D0Q4SD
  INTEDE ID: DR0592
  ACDINA ID: D00235
• Repurposed Drugs (RPD): Click to Jump to the Detailed RPD Information of This Drug

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Mineralocorticoid receptor (MR)	TT26PHO	MCR_HUMAN	Modulator	[6]
HUMAN mineralocorticoid receptor (MR)	TT9P1CK	MCR_HUMAN	Antagonist	[2]

Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
Cytochrome P450 3A4 (CYP3A4)	DE4LYSA	CP3A4_HUMAN	Substrate	[7]
Cytochrome P450 3A5 (CYP3A5)	DEIBDNY	CP3A5_HUMAN	Substrate	[8]

Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
Cytochrome P450 3A4 (CYP3A4)	OTQGYY83	CP3A4_HUMAN	Regulation of Drug Effects	[8]
Cytochrome P450 3A5 (CYP3A5)	OTSXFBXB	CP3A5_HUMAN	Regulation of Drug Effects	[8]

Molecular Expression Atlas of This Drug

• The Studied Disease: Heart failure
• ICD Disease Classification: BD10-BD13

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Mineralocorticoid receptor (MR)	DTT	NR3C2	7.31E-01	-5.31E-04	-1.53E-03
Cytochrome P450 3A5 (CYP3A5)	DME	CYP3A5	8.58E-01	-3.73E-03	-1.00E-02
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	2.76E-01	-4.64E-01	-9.16E-01

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Eplerenone (Comorbidity)

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Arn-509	DMT81LZ	Minor	Increased metabolism of Eplerenone caused by Arn-509 mediated induction of CYP450 enzyme.	Acute myeloid leukaemia [2A60]	[9]
Dronedarone	DMA8FS5	Major	Decreased metabolism of Eplerenone caused by Dronedarone mediated inhibition of CYP450 enzyme.	Angina pectoris [BA40]	[10]
Posaconazole	DMUL5EW	Major	Decreased metabolism of Eplerenone caused by Posaconazole mediated inhibition of CYP450 enzyme.	Aspergillosis [1F20]	[11]
Dalfopristin	DM4LTKV	Major	Decreased metabolism of Eplerenone caused by Dalfopristin mediated inhibition of CYP450 enzyme.	Bacterial infection [1A00-1C4Z]	[10]
Clarithromycin	DM4M1SG	Major	Decreased metabolism of Eplerenone caused by Clarithromycin mediated inhibition of CYP450 enzyme.	Bacterial infection [1A00-1C4Z]	[11]
Troleandomycin	DMUZNIG	Major	Decreased metabolism of Eplerenone caused by Troleandomycin mediated inhibition of CYP450 enzyme.	Bacterial infection [1A00-1C4Z]	[11]
Telithromycin	DMZ4P3A	Major	Decreased metabolism of Eplerenone caused by Telithromycin mediated inhibition of CYP450 enzyme.	Bacterial infection [1A00-1C4Z]	[11]
Cariprazine	DMJYDVK	Moderate	Additive hypotensive effects by the combination of Eplerenone and Cariprazine.	Bipolar disorder [6A60]	[12]
Phenylbutazone	DMAYL0T	Moderate	Antagonize the effect of Eplerenone when combined with Phenylbutazone.	Chronic pain [MG30]	[13]
Ketoprofen	DMRKXPT	Moderate	Increased risk of hyperkalemia by the combination of Eplerenone and Ketoprofen.	Chronic pain [MG30]	[13]
Mifepristone	DMGZQEF	Major	Decreased metabolism of Eplerenone caused by Mifepristone mediated inhibition of CYP450 enzyme.	Cushing syndrome [5A70]	[14]
Ivacaftor	DMZC1HS	Moderate	Decreased metabolism of Eplerenone caused by Ivacaftor mediated inhibition of CYP450 enzyme.	Cystic fibrosis [CA25]	[15]
MK-8228	DMOB58Q	Major	Decreased metabolism of Eplerenone caused by MK-8228 mediated inhibition of CYP450 enzyme.	Cytomegaloviral disease [1D82]	[10]
Nefazodone	DM4ZS8M	Major	Decreased metabolism of Eplerenone caused by Nefazodone mediated inhibition of CYP450 enzyme.	Depression [6A70-6A7Z]	[11]
Selegiline	DM6034S	Moderate	Additive hypotensive effects by the combination of Eplerenone and Selegiline.	Depression [6A70-6A7Z]	[16]
Isocarboxazid	DMAF1NB	Moderate	Additive hypotensive effects by the combination of Eplerenone and Isocarboxazid.	Depression [6A70-6A7Z]	[16]
Tranylcypromine	DMGB5RE	Moderate	Additive hypotensive effects by the combination of Eplerenone and Tranylcypromine.	Depression [6A70-6A7Z]	[16]
OPC-34712	DMHG57U	Moderate	Additive hypotensive effects by the combination of Eplerenone and OPC-34712.	Depression [6A70-6A7Z]	[12]
Phenelzine	DMHIDUE	Moderate	Additive hypotensive effects by the combination of Eplerenone and Phenelzine.	Depression [6A70-6A7Z]	[16]
Primidone	DM0WX6I	Minor	Increased metabolism of Eplerenone caused by Primidone mediated induction of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[9]
Stiripentol	DMMSDOY	Major	Decreased metabolism of Eplerenone caused by Stiripentol mediated inhibition of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[10]
Fosphenytoin	DMOX3LB	Minor	Increased metabolism of Eplerenone caused by Fosphenytoin mediated induction of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[9]
Rufinamide	DMWE60C	Moderate	Increased metabolism of Eplerenone caused by Rufinamide mediated induction of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[17]
Phenobarbital	DMXZOCG	Minor	Increased metabolism of Eplerenone caused by Phenobarbital mediated induction of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[9]
Mefenamic acid	DMK7HFI	Moderate	Antagonize the effect of Eplerenone when combined with Mefenamic acid.	Female pelvic pain [GA34]	[13]
Itraconazole	DMCR1MV	Major	Decreased metabolism of Eplerenone caused by Itraconazole mediated inhibition of CYP450 enzyme.	Fungal infection [1F29-1F2F]	[11]
Miconazole	DMPMYE8	Moderate	Decreased metabolism of Eplerenone caused by Miconazole mediated inhibition of CYP450 enzyme.	Fungal infection [1F29-1F2F]	[18]
Ketoconazole	DMPZI3Q	Major	Decreased metabolism of Eplerenone caused by Ketoconazole mediated inhibition of CYP450 enzyme.	Fungal infection [1F29-1F2F]	[11]
Boceprevir	DMBSHMF	Major	Decreased metabolism of Eplerenone caused by Boceprevir mediated inhibition of CYP450 enzyme.	Hepatitis virus infection [1E50-1E51]	[11]
Telaprevir	DMMRV29	Major	Decreased metabolism of Eplerenone caused by Telaprevir mediated inhibition of CYP450 enzyme.	Hepatitis virus infection [1E50-1E51]	[11]
Rifampin	DMA8J1G	Minor	Increased metabolism of Eplerenone caused by Rifampin mediated induction of CYP450 enzyme.	HIV-infected patients with tuberculosis [1B10-1B14]	[11]
Procarbazine	DMIK367	Moderate	Additive hypotensive effects by the combination of Eplerenone and Procarbazine.	Hodgkin lymphoma [2B30]	[16]
Delavirdine	DM3NF5G	Major	Decreased metabolism of Eplerenone caused by Delavirdine mediated inhibition of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[11]
Fosamprenavir	DM4W9B3	Major	Decreased metabolism of Eplerenone caused by Fosamprenavir mediated inhibition of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[11]
Cobicistat	DM6L4H2	Major	Decreased metabolism of Eplerenone caused by Cobicistat mediated inhibition of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[11]
Saquinavir	DMG814N	Major	Decreased metabolism of Eplerenone caused by Saquinavir mediated inhibition of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[11]
Etravirine	DMGV8QU	Moderate	Increased metabolism of Eplerenone caused by Etravirine mediated induction of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[19]
Amprenavir	DMLMXE0	Major	Decreased metabolism of Eplerenone caused by Amprenavir mediated inhibition of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[11]
Darunavir	DMN3GCH	Major	Decreased metabolism of Eplerenone caused by Darunavir mediated inhibition of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[10]
Atazanavir	DMSYRBX	Major	Decreased metabolism of Eplerenone caused by Atazanavir mediated inhibition of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[11]
Eprosartan	DM07K2I	Moderate	Increased risk of hyperkalemia by the combination of Eplerenone and Eprosartan.	Hypertension [BA00-BA04]	[10]
Captopril	DM458UM	Moderate	Increased risk of hyperkalemia by the combination of Eplerenone and Captopril.	Hypertension [BA00-BA04]	[10]
TAK-491	DMCF6SX	Moderate	Increased risk of hyperkalemia by the combination of Eplerenone and TAK-491.	Hypertension [BA00-BA04]	[10]
Perindopril	DMOPZDT	Moderate	Increased risk of hyperkalemia by the combination of Eplerenone and Perindopril.	Hypertension [BA00-BA04]	[10]
Quinapril	DMR8H31	Moderate	Increased risk of hyperkalemia by the combination of Eplerenone and Quinapril.	Hypertension [BA00-BA04]	[10]
Telmisartan	DMS3GX2	Moderate	Increased risk of hyperkalemia by the combination of Eplerenone and Telmisartan.	Hypertension [BA00-BA04]	[10]
Irbesartan	DMTP1DC	Moderate	Increased risk of hyperkalemia by the combination of Eplerenone and Irbesartan.	Hypertension [BA00-BA04]	[10]
Lisinopril	DMUOK4C	Moderate	Increased risk of hyperkalemia by the combination of Eplerenone and Lisinopril.	Hypertension [BA00-BA04]	[10]
Potassium chloride	DMMTAJC	Major	Increased risk of hyperkalemia by the combination of Eplerenone and Potassium chloride.	Hypo-kalaemia [5C77]	[20]
Conivaptan	DM1V329	Major	Decreased metabolism of Eplerenone caused by Conivaptan mediated inhibition of CYP450 enzyme.	Hypo-osmolality/hyponatraemia [5C72]	[11]
Tolvaptan	DMIWFRL	Moderate	Increased risk of hyperkalemia by the combination of Eplerenone and Tolvaptan.	Hypo-osmolality/hyponatraemia [5C72]	[21]
Meclofenamic acid	DM05FXR	Moderate	Antagonize the effect of Eplerenone when combined with Meclofenamic acid.	Inflammatory spondyloarthritis [FA92]	[22]
Berotralstat	DMWA2DZ	Major	Decreased metabolism of Eplerenone caused by Berotralstat mediated inhibition of CYP450 enzyme.	Innate/adaptive immunodeficiency [4A00]	[10]
Propiomazine	DMKY8V1	Moderate	Additive hypotensive effects by the combination of Eplerenone and Propiomazine.	Insomnia [7A00-7A0Z]	[12]
ITI-007	DMUQ1DO	Moderate	Additive hypotensive effects by the combination of Eplerenone and ITI-007.	Insomnia [7A00-7A0Z]	[12]
Crizotinib	DM4F29C	Major	Decreased metabolism of Eplerenone caused by Crizotinib mediated inhibition of CYP450 enzyme.	Lung cancer [2C25]	[10]
Brigatinib	DM7W94S	Moderate	Increased metabolism of Eplerenone caused by Brigatinib mediated induction of CYP450 enzyme.	Lung cancer [2C25]	[23]
Ceritinib	DMB920Z	Major	Decreased metabolism of Eplerenone caused by Ceritinib mediated inhibition of CYP450 enzyme.	Lung cancer [2C25]	[11]
PF-06463922	DMKM7EW	Moderate	Increased metabolism of Eplerenone caused by PF-06463922 mediated induction of CYP450 enzyme.	Lung cancer [2C25]	[24]
Selpercatinib	DMZR15V	Moderate	Decreased metabolism of Eplerenone caused by Selpercatinib mediated inhibition of CYP450 enzyme.	Lung cancer [2C25]	[17]
Idelalisib	DM602WT	Major	Decreased metabolism of Eplerenone caused by Idelalisib mediated inhibition of CYP450 enzyme.	Mature B-cell leukaemia [2A82]	[11]
IPI-145	DMWA24P	Major	Decreased metabolism of Eplerenone caused by IPI-145 mediated inhibition of CYP450 enzyme.	Mature B-cell leukaemia [2A82]	[10]
Dabrafenib	DMX6OE3	Moderate	Increased metabolism of Eplerenone caused by Dabrafenib mediated induction of CYP450 enzyme.	Melanoma [2C30]	[17]
Exjade	DMHPRWG	Moderate	Decreased metabolism of Eplerenone caused by Exjade mediated inhibition of CYP450 enzyme.	Mineral absorption/transport disorder [5C64]	[25]
Ozanimod	DMT6AM2	Moderate	Additive hypotensive effects by the combination of Eplerenone and Ozanimod.	Multiple sclerosis [8A40]	[16]
Modafinil	DMYILBE	Minor	Increased metabolism of Eplerenone caused by Modafinil mediated induction of CYP450 enzyme.	Narcolepsy [7A20]	[26]
Promethazine	DM6I5GR	Moderate	Additive hypotensive effects by the combination of Eplerenone and Promethazine.	Nausea/vomiting [MD90]	[12]
Netupitant	DMEKAYI	Major	Decreased metabolism of Eplerenone caused by Netupitant mediated inhibition of CYP450 enzyme.	Nausea/vomiting [MD90]	[10]
Naproxen	DMZ5RGV	Moderate	Antagonize the effect of Eplerenone when combined with Naproxen.	Osteoarthritis [FA00-FA05]	[13]
Aspirin	DM672AH	Moderate	Antagonize the effect of Eplerenone when combined with Aspirin.	Pain [MG30-MG3Z]	[22]
Etodolac	DM6WJO9	Moderate	Antagonize the effect of Eplerenone when combined with Etodolac.	Pain [MG30-MG3Z]	[13]
Diflunisal	DM7EN8I	Moderate	Antagonize the effect of Eplerenone when combined with Diflunisal.	Pain [MG30-MG3Z]	[13]
Ibuprofen	DM8VCBE	Moderate	Antagonize the effect of Eplerenone when combined with Ibuprofen.	Pain [MG30-MG3Z]	[13]
Safinamide	DM0YWJC	Moderate	Additive hypotensive effects by the combination of Eplerenone and Safinamide.	Parkinsonism [8A00]	[16]
Rasagiline	DM3WKQ4	Moderate	Additive hypotensive effects by the combination of Eplerenone and Rasagiline.	Parkinsonism [8A00]	[16]
Abametapir	DM2RX0I	Moderate	Decreased metabolism of Eplerenone caused by Abametapir mediated inhibition of CYP450 enzyme.	Pediculosis [1G00]	[27]
Lefamulin	DME6G97	Moderate	Decreased metabolism of Eplerenone caused by Lefamulin mediated inhibition of CYP450 enzyme.	Pneumonia [CA40]	[28]
Choline salicylate	DM8P137	Moderate	Antagonize the effect of Eplerenone when combined with Choline salicylate.	Postoperative inflammation [1A00-CA43]	[13]
Bromfenac	DMKB79O	Moderate	Antagonize the effect of Eplerenone when combined with Bromfenac.	Postoperative inflammation [1A00-CA43]	[13]
Lonafarnib	DMGM2Z6	Major	Decreased metabolism of Eplerenone caused by Lonafarnib mediated inhibition of CYP450 enzyme.	Premature ageing appearance [LD2B]	[11]
Enzalutamide	DMGL19D	Minor	Increased metabolism of Eplerenone caused by Enzalutamide mediated induction of CYP450 enzyme.	Prostate cancer [2C82]	[9]
Levomepromazine	DMIKFEL	Moderate	Additive hypotensive effects by the combination of Eplerenone and Levomepromazine.	Psychotic disorder [6A20-6A25]	[12]
Temsirolimus	DMS104F	Moderate	Increased plasma concentrations of Eplerenone and Temsirolimus due to competitive inhibition of the same metabolic pathway.	Renal cell carcinoma [2C90]	[29]
Salsalate	DM13P4C	Moderate	Antagonize the effect of Eplerenone when combined with Salsalate.	Rheumatoid arthritis [FA20]	[13]
Meloxicam	DM2AR7L	Moderate	Antagonize the effect of Eplerenone when combined with Meloxicam.	Rheumatoid arthritis [FA20]	[13]
Oxaprozin	DM9UB0P	Moderate	Antagonize the effect of Eplerenone when combined with Oxaprozin.	Rheumatoid arthritis [FA20]	[13]
Flurbiprofen	DMGN4BY	Moderate	Antagonize the effect of Eplerenone when combined with Flurbiprofen.	Rheumatoid arthritis [FA20]	[13]
Quetiapine	DM1N62C	Moderate	Additive hypotensive effects by the combination of Eplerenone and Quetiapine.	Schizophrenia [6A20]	[12]
Mesoridazine	DM2ZGAN	Moderate	Additive hypotensive effects by the combination of Eplerenone and Mesoridazine.	Schizophrenia [6A20]	[12]
Aripiprazole	DM3NUMH	Moderate	Additive hypotensive effects by the combination of Eplerenone and Aripiprazole.	Schizophrenia [6A20]	[12]
Iloperidone	DM6AUFY	Moderate	Additive hypotensive effects by the combination of Eplerenone and Iloperidone.	Schizophrenia [6A20]	[12]
Paliperidone	DM7NPJS	Moderate	Additive hypotensive effects by the combination of Eplerenone and Paliperidone.	Schizophrenia [6A20]	[12]
Perphenazine	DMA4MRX	Moderate	Additive hypotensive effects by the combination of Eplerenone and Perphenazine.	Schizophrenia [6A20]	[12]
Molindone	DMAH70G	Moderate	Additive hypotensive effects by the combination of Eplerenone and Molindone.	Schizophrenia [6A20]	[12]
Thiothixene	DMDINC4	Moderate	Additive hypotensive effects by the combination of Eplerenone and Thiothixene.	Schizophrenia [6A20]	[12]
Trifluoperazine	DMKBYWI	Moderate	Additive hypotensive effects by the combination of Eplerenone and Trifluoperazine.	Schizophrenia [6A20]	[12]
Risperidone	DMN6DXL	Moderate	Additive hypotensive effects by the combination of Eplerenone and Risperidone.	Schizophrenia [6A20]	[12]
Amisulpride	DMSJVAM	Moderate	Additive hypotensive effects by the combination of Eplerenone and Amisulpride.	Schizophrenia [6A20]	[12]
Asenapine	DMSQZE2	Moderate	Additive hypotensive effects by the combination of Eplerenone and Asenapine.	Schizophrenia [6A20]	[12]
Salicyclic acid	DM2F8XZ	Moderate	Increased risk of hyperkalemia by the combination of Eplerenone and Salicyclic acid.	Seborrhoeic dermatitis [EA81]	[22]
Voxelotor	DMCS6M5	Major	Decreased metabolism of Eplerenone caused by Voxelotor mediated inhibition of CYP450 enzyme.	Sickle-cell disorder [3A51]	[10]
Telotristat ethyl	DMDIYFZ	Moderate	Increased metabolism of Eplerenone caused by Telotristat ethyl mediated induction of CYP450 enzyme.	Small intestine developmental anomaly [DA90]	[17]
Larotrectinib	DM26CQR	Moderate	Decreased metabolism of Eplerenone caused by Larotrectinib mediated inhibition of CYP450 enzyme.	Solid tumour/cancer [2A00-2F9Z]	[11]
Armodafinil	DMGB035	Minor	Increased metabolism of Eplerenone caused by Armodafinil mediated induction of CYP450 enzyme.	Solid tumour/cancer [2A00-2F9Z]	[26]
LEE011	DMMX75K	Major	Decreased metabolism of Eplerenone caused by LEE011 mediated inhibition of CYP450 enzyme.	Solid tumour/cancer [2A00-2F9Z]	[10]
Pitolisant	DM8RFNJ	Moderate	Increased metabolism of Eplerenone caused by Pitolisant mediated induction of CYP450 enzyme.	Somnolence [MG42]	[17]
Fostamatinib	DM6AUHV	Moderate	Decreased metabolism of Eplerenone caused by Fostamatinib mediated inhibition of CYP450 enzyme.	Thrombocytopenia [3B64]	[30]
Sirolimus	DMGW1ID	Moderate	Increased plasma concentrations of Eplerenone and Sirolimus due to competitive inhibition of the same metabolic pathway.	Transplant rejection [NE84]	[29]
Tacrolimus	DMZ7XNQ	Moderate	Increased plasma concentrations of Eplerenone and Tacrolimus due to competitive inhibition of the same metabolic pathway.	Transplant rejection [NE84]	[20]
Methdilazine	DMAUHQX	Moderate	Additive hypotensive effects by the combination of Eplerenone and Methdilazine.	Vasomotor/allergic rhinitis [CA08]	[12]
Trimeprazine	DMEMV9D	Moderate	Additive hypotensive effects by the combination of Eplerenone and Trimeprazine.	Vasomotor/allergic rhinitis [CA08]	[31]
Amiodarone	DMUTEX3	Major	Decreased metabolism of Eplerenone caused by Amiodarone mediated inhibition of CYP450 enzyme.	Ventricular tachyarrhythmia [BC71]	[10]

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG

DIG Name	DIG ID	PubChem CID	Functional Classification
Hydrazine yellow	E00409	164825	Colorant
Sodium lauryl sulfate	E00464	3423265	Emulsifying agent; Modified-release agent; Penetration agent; Solubilizing agent; Surfactant; lubricant
Sunset yellow FCF	E00255	17730	Colorant
Beta-D-lactose	E00099	6134	Diluent; Dry powder inhaler carrier; Lyophilization aid
Carmellose sodium	E00625	Not Available	Disintegrant
Eisenoxyd	E00585	56841934	Colorant
Ferric hydroxide oxide yellow	E00539	23320441	Colorant
Lactose monohydrate	E00393	104938	Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate	E00208	11177	lubricant
Polysorbate 80	E00665	Not Available	Dispersing agent; Emollient; Emulsifying agent; Plasticizing agent; Solubilizing agent; Surfactant; Suspending agent
Talc	E00520	16211421	Anticaking agent; Diluent; Glidant; lubricant
Titanium dioxide	E00322	26042	Coating agent; Colorant; Opacifying agent
Triacetin	E00080	5541	Humectant; Plasticizing agent; Solvent
Vinylpyrrolidone	E00668	Not Available	Binding agent; Coating agent; Disintegrant; Film/membrane-forming agent; Solubilizing agent; Suspending agent

Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Eplerenone 25 mg tablet	25 mg	Oral Tablet	Oral
Eplerenone 50 mg tablet	50 mg	Oral Tablet	Oral

Jump to Detail Pharmaceutical Formulation Page of This Drug

References

• [1] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2876).
• [2] Network-based drug repurposing for novel coronavirus 2019-nCoV/SARS-CoV-2. Cell Discov. 2020 Mar 16;6:14.
• [3] BDDCS applied to over 900 drugs
• [4] Critical Evaluation of Human Oral Bioavailability for Pharmaceutical Drugs by Using Various Cheminformatics Approaches
• [5] Estimating the safe starting dose in phase I clinical trials and no observed effect level based on QSAR modeling of the human maximum recommended daily dose
• [6] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [7] Eplerenone: a selective aldosterone receptor antagonist for hypertension and heart failure. Heart Dis. 2003 Sep-Oct;5(5):354-63.
• [8] The relative role of CYP3A4 and CYP3A5 in eplerenone metabolism. Toxicol Lett. 2019 Oct 15;315:9-13.
• [9] Agencia Espaola de Medicamentos y Productos Sanitarios Healthcare "Centro de informacion online de medicamentos de la AEMPS - CIMA.".
• [10] Product Information. Inspra (eplerenone). Searle, Chicago, IL.
• [11] Cerner Multum, Inc. "Australian Product Information.".
• [12] Aronowitz JS, Chakos MH, Safferman AZ, Lieberman JA "Syncope associated with the combination of clozapine and enalapril." J Clin Psychopharmacol 14 (1994): 429-30. [PMID: 7884028]
• [13] Abdel-Haq B, Magagna A, Favilla S, Salvetti A "Hemodynamic and humoral interactions between perindopril and indomethacin in essential hypertensive subjects." J Cardiovasc Pharmacol 18 (1991): s33-6. [PMID: 1725198]
• [14] He K, Woolf TF, Hollenberg PF "Mechanism-based inactivation of cytochrome P-450-3A4 by mifepristone (RU486)." J Pharmacol Exp Ther 288 (1999): 791-7. [PMID: 9918590]
• [15] Product Information. Kalydeco (ivacaftor). Vertex Pharmaceuticals, Cambridge, MA.
• [16] Ban TA "Drug interactions with psychoactive drugs." Dis Nerv Syst 36 (1975): 164-6. [PMID: 1116424]
• [17] Cerner Multum, Inc. "UK Summary of Product Characteristics.".
• [18] Product Information. ORAVIG (miconazole). Strativa Pharmaceuticals, a Division of Par Pharmaceuticals, Inc., Woodcliff Lake, NJ.
• [19] Product Information. Intelence (etravirine). Ortho Biotech Inc, Bridgewater, NJ.
• [20] Marcy TR, Ripley TL "Aldosterone antagonists in the treatment of heart failure." Am J Health Syst Pharm 63 (2006): 49-58. [PMID: 16373465]
• [21] Product Information. Samsca (tolvaptan). Otsuka American Pharmaceuticals Inc, Rockville, MD.
• [22] Radack KL, Deck CC, Bloomfield SS "Ibuprofen interferes with the efficacy of antihypertensive drugs: a randomized, double-blind, placebo-controlled trial of ibuprofen compared with acetaminophen." Ann Intern Med 107 (1987): 628-35. [PMID: 2889416]
• [23] Product Information. Alunbrig (brigatinib). Ariad Pharmaceuticals Inc, Cambridge, MA.
• [24] Product Information. Lorbrena (lorlatinib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
• [25] Product Information. Exjade (deferasirox). Novartis Pharmaceuticals, East Hanover, NJ.
• [26] Doherty MM, Charman WN "The mucosa of the small intestine: how clinically relevant as an organ of drug metabolism?" Clin Pharmacokinet 41 (2002): 235-53. [PMID: 11978143]
• [27] Product Information. Xeglyze (abametapir topical). Dr. Reddy's Laboratories Inc, Upper Saddle River, NJ.
• [28] Product Information. Xenleta (lefamulin). Nabriva Therapeutics US, Inc., King of Prussia, PA.
• [29] Product Information. Prograf (tacrolimus). Fujisawa, Deerfield, IL.
• [30] Product Information. Tavalisse (fostamatinib). Rigel Pharmaceuticals, South San Francisco, CA.
• [31] Product Information. Clozaril (clozapine). Novartis Pharmaceuticals, East Hanover, NJ.